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Voltage-dependent calcium channel subunit alpha2-delta2 (α2δ-2)

Target
α2δ-2
Molecular classification
Voltage-gated Calcium Channel Auxiliary Subunit
01

Overview

The voltage-dependent calcium channel subunit alpha2-delta2 (α2δ-2) is an auxiliary protein component of high-voltage-activated (HVA) calcium channels, encoded by the CACNA2D2 gene. It regulates calcium current density, modulates activation and inactivation kinetics, and influences trafficking and surface expression of associated calcium channels like P/Q-, N-, and L-type. It plays a role in synapse organization and, in neurons, limits axon growth/regeneration. α2δ-2 is a target for gabapentinoid drugs used to treat epilepsy and neuropathic pain.

02

Mechanism of action

Gabapentinoids bind to the α2δ subunits, especially isoforms 1 and 2, of voltage-dependent calcium channels, modulating calcium influx and reducing the release of excitatory neurotransmitters.

03

Biological functions

Regulation of calcium current densityModulation of calcium channel kineticsRegulation of trafficking and surface expression of calcium channelsSynapse organizationRegulation of axon growth/regeneration
04

Disease associations

EpilepsyNeuropathic painDiabetic neuropathyNeuralgiaInflammation-related painChemotherapy-induced peripheral neuropathyCentral nervous system disorders
05

Interacting drugs

Gabapentin

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